模拟生物膜色谱用于预测药物的小肠吸收

Prediction of Intestinal Absorption of Drugs with Mimetic Biomembrane Chromatography

采用涂敷磷脂的硅胶为模拟生物膜色谱固定相，与传统的凝胶载体相比固定相的机械强度及磷脂固载能力均有较大提高，且有较好的稳定性 研究发现氢化可的松等６种药物在模拟生物膜色谱上ｐＨ ５．４、ｐＨ ７．０及ｐＨ ７．４三种缓冲环境下的色谱保留值迭加的结果能够与药物的肠吸收指数较好的拟合，线性相关系数为０ ９３６５，该结果高于单－ｐＨ条件下的拟合结果，并将此结果与药物在Ｃ１８反相色谱上的保留值及辛醇－水系统下的分配系数与药物的小肠吸收的拟合结果进行比较，表明与这两种模型相比模拟生物膜色谱预测药物的小肠吸收有更高的准确度。

Silica coated lecithin was used as solid phase, the amount of lecithin coated and mechanical strength of the packing were all superior to gel, the traditional material used in the process of immobilization of liposome, and the stability of lecithin coated on silica was also good. The retention values of six drugs on mimetic biomembrane chromatography have been measured with three different pH buffers ( pH 5.4, pH 7.0 and pH 7.4) as mobile phase. The weighed retention values have been proposed to simulate the intestinal absorption of drugs. It was observed that the linear correlation coefficient (r = 0.9365) was higher than that with single buffer as mobile phase. Comparing the result above with that of correlation between retention of drugs on C-18 reversed phase chromatographic column and distributive coefficient of drugs in octanol-water system and intestinal absorption, it was observed that mimetic biomembrane chromatography had better precision than other two models when they were used to predict intestinal absorption of drugs.